Assay Detail
Binding
CHEMBL922845
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Inhibition of [3H]5HT uptake in SERT in rat cerebral cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 5.53 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.04 |
| CHEMBL258724 | — | — | 1 | 7.04 |
| CHEMBL258725 | — | — | 1 | 5.86 |
| CHEMBL260682 | — | — | 1 | 5.83 |
| CHEMBL258511 | — | — | 1 | 5.59 |
| CHEMBL261736 | — | — | 1 | 5.54 |
| CHEMBL265454 | — | — | 1 | 5.13 |
| CHEMBL408950 | — | — | 1 | 5.13 |
| CHEMBL412263 | — | — | 1 | 5.02 |
| CHEMBL410244 | — | — | 1 | 4.99 |
| CHEMBL260151 | — | — | 1 | 4.95 |
| CHEMBL263636 | — | — | 1 | 4.92 |
| CHEMBL409881 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281594 | VANOXERINE | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL258724 | — | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL258725 | — | Ki | = | 1391.0 | nM | 5.86 |
| CHEMBL260682 | — | Ki | = | 1484.0 | nM | 5.83 |
| CHEMBL258511 | — | Ki | = | 2596.0 | nM | 5.59 |
| CHEMBL261736 | — | Ki | = | 2895.0 | nM | 5.54 |
| CHEMBL265454 | — | Ki | = | 7344.0 | nM | 5.13 |
| CHEMBL408950 | — | Ki | = | 7414.0 | nM | 5.13 |
| CHEMBL412263 | — | Ki | = | 9508.0 | nM | 5.02 |
| CHEMBL410244 | — | Ki | = | 10336.0 | nM | 4.99 |
| CHEMBL260151 | — | Ki | = | 11216.0 | nM | 4.95 |
| CHEMBL263636 | — | Ki | = | 11884.0 | nM | 4.92 |
| CHEMBL409881 | — | Ki | = | 12904.0 | nM | 4.89 |